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Indane dimers for use in the treatment of autoimmune inflammatory disease

a technology of autoimmune inflammatory disease and dimers, which is applied in the field of compounds, can solve the problems of no longer recommended use of these drugs to maintain remission in cd, no benefit in maintaining remission, and systemic absorption, and achieve the effect of improving the availability of medicaments

Inactive Publication Date: 2015-05-21
VENANTIUS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent text is about making capsules by mixing powder, liquid, or suspension with a gelatin shell and adding other ingredients to improve their availability and performance when taken. Examples of ingredients include lubricants, disintegrating agents, and coloring agents. The text also mentions common binders and lubricants used in this process.

Problems solved by technology

However, while the use of aminosalycilates in UC provides considerable benefit, both in inducing remission in mild to moderate disease and in preventing relapse, the usefulness of these drugs to maintain remission in CD is questionable and is no longer recommended.
The mainstay of treatment of active disease is a corticosteroid, commonly used for limited periods to return both UC and CD patients to remission, though budesonide, designed for topical administration with limited systemic absorption, has no benefit in maintaining remission.
Alternatives, such as the immunosuppressive drugs azathioprine and mercaptopurine, together with methotrexate and cyclosporine have limited efficacy and the capability of inducing grave adverse effects.
However, many patients fail to respond to anti-TNFα therapy, either due to their particular phenotype or by the production of autoantibodies.

Method used

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  • Indane dimers for use in the treatment of autoimmune inflammatory disease
  • Indane dimers for use in the treatment of autoimmune inflammatory disease
  • Indane dimers for use in the treatment of autoimmune inflammatory disease

Examples

Experimental program
Comparison scheme
Effect test

experiment 1

Compounds 2-6

Mice

[0289]Specific Pathogen-Free BALB / c mice, 6-8 weeks of age, were obtained from a commercial supplier (Harlan UK). Mice were fed irradiated diet and housed in individually ventilated cages (Tecniplast UK) under positive pressure.

DSS treatment

[0290]DSS (5%) was dissolved in drinking water. Compounds were administered orally at a dose of 10 mg / kg or 30 mg / kg on days 0-7, and mice were culled on day 8 or day 9, depending on the severity of the disease. The mice were checked each day for morbidity and the weight of individual mice was recorded. Induction of colitis was determined upon autopsy, length of colon and histology. Colons were recovered and stored at −20° C. for immunological analysis. All of the compounds and experimental groups are randomly alphabetically labelled. Throughout experiments all data recording was performed in a blind manner. The codes on boxes / groups were not broken until after the data was analysed i.e. boxes labelled A, B, C etc were identified...

experiment 2

Compounds 31 and 47.

1. Procedures

2.1 Animals and Caging

[0318]A total of 90 BDF 1 (H. Pylori-free, murine norovirus-free) male mice (Harlan Laboratories, UK) were used in the study. Animals were 8-10 weeks old on supply and used at 10-12 weeks of age. All mice were held in individually ventilated cages (IVCs) in an SPF (Specific Pathogen Free) barrier unit. The animals were identified by numbered cages and by ear punches.

2.2 Diet and Animal Welfare

[0319]The animals were fed Rat and Mouse Expanded diet from B & K. Both feed and water (from drinking bottles) were available ad libitum. There was a constant room temperature of 21±2° C. and a mean relative humidity of 55±10%. The day-night cycle was constant, with light and dark phases of 12 hours each. Animal health was monitored daily and cages were cleaned at regular intervals.

2.3 Groups, Dosages, Administration and Formulations

[0320]Mice were randomised into study groups. All the mice in any one cage received the same treatment and we...

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Abstract

Compounds particularly for use in an autoimmune inflammatory disease and especially the treatment of inflammatory bowel disease have the absolute stereochemistry and formula:In some cases R1 is leucine and R is selected from: OH, OCH3, OCH2CH3, OCH2CH2CH3, NH2, NHCH2CH2OH, NHCH3, N(CH3)2, NH(4-OH-3-benzoic acid).

Description

[0001]This invention relates to compounds particularly for use in the autoimmune inflammatory disease and specifically the treatment of inflammatory bowel disease.INTRODUCTION[0002]Cytokines can be produced by various cell populations and have been shown to augment or limit immune responses to pathogens and influence the autoimmune response. One family of cytokines, which uses the common receptor gamma chain (cc), a component of receptors for interleukin (IL)-2, IL-4, IL-7, IL-9, IL-15 and IL-21, has been classically defined as growth and survival factors.[0003]IL-2 production can induce an immune response by promoting the proliferation and generation of CD4+ Th1, CD4+ Th2 and CD8+ CTL effector cells. Many of the immunosuppressive drugs used in the treatment of autoimmune diseases and organ transplant rejection, such as corticosteroids and immune suppressive drugs (ciclosporin, tacrolimus) work by inhibiting the production of IL-2 by antigen-activated T cells. Others (sirolimus) blo...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): C07C65/17C07C237/32C07C229/12C07C229/38C07C69/78C07C235/42
CPCC07C65/17C07C69/78C07C235/42C07C2102/08C07C229/38C07C237/32C07C229/12C07C65/19C07C69/76C07C229/08C07B2200/07C07C2602/08A61P29/00
Inventor FRANKISH, NEILSHERIDAN, HELEN
Owner VENANTIUS